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Crisaborole (AN2728) PDE inhibitor

Name: Crisaborole (AN2728)
SKU: S5014
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5014

Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.

Chemical Structure

Molecular Weight: 251.05

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S501401 DMSO]50 mg/mL]false]]]false]]]false Purity: 98%

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Chemical Information, Storage & Stability

Molecular Weight	251.05	Formula	C₁₄H₁₀BNO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	906673-24-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	B1(C2=C(CO1)C=C(C=C2)OC3=CC=C(C=C3)C#N)O

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (199.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.5mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.36mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PDE4 ^[1] (Cell-free assay)
In vivo	Crisaborole is well tolerated and not tumorigenic in mice^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/28416366/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04800185	Completed	Atopic Dermatitis\|Atopic Dermatitis Eczema	University of California Irvine\|Pfizer	March 23 2021	Early Phase 1
NCT03954158	Completed	Atopic Dermatitis	Pfizer	June 15 2019	Phase 2
NCT03260595	Completed	Healthy\|Atopic Dermatitis	Pfizer	September 13 2017	Phase 1
NCT01652885	Completed	Dermatitis Atopic	Pfizer	July 2012	Phase 1\|Phase 2

Tech Support

Handling Instructions

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